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Preparation method of carrier-free [*X]MXBG

A carrier-free, trialkyltin technology, applied in the preparation of organic compounds, organic chemical methods, chemical instruments and methods, etc., can solve the problems of many impurities, complicated steps, low yield, etc., and achieve low impurity content, steps Simple, high-yield effect

Inactive Publication Date: 2015-07-08
JIANGSU INST OF NUCLEAR MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] For this reason, the technical problem to be solved by the present invention is that the productive rate of carrier-free [*X]MXBG in the prior art is low, the steps are complicated, and there are many impurities, etc. Preparation method of carrier [*X]MXBG

Method used

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  • Preparation method of carrier-free [*X]MXBG
  • Preparation method of carrier-free [*X]MXBG
  • Preparation method of carrier-free [*X]MXBG

Examples

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preparation example Construction

[0066] The preparation routes of the following examples of the present invention are as follows:

[0067]

Embodiment 1

[0069] The preparation of this embodiment has no carrier [ 131 I] The method of MIBG is as follows:

[0070] (1) Synthesis of 3-(tributyltin base)-benzylguanidine shown in the formula A-II

[0071] Take 500mg (1.48mmol) of the bicarbonate of m-iodobenzylguanidine represented by the formula A-I and dissolve it in 10mL of DMSO solution, then add 947mg (1.63mmol) of bis(tributyltin) and mix well, and dissolve the whole In 30mL of 1,4-dioxane, then add 104mg (0.15mmol) of bistriphenylphosphine palladium dichloride, and control the temperature at 100°C to carry out stille organotin reaction until the solution turns black and the color of the solution is Without further deepening, spin dry the obtained above solution, take ethyl acetate to dissolve the spin-dried residue, then wash the solution with water, spin dry again, take methanol to dissolve the residue after spin-dry again, and then use n-hexane Wash the dissolving solution, then dry, and the 3-(tributyltin base)-benzylguan...

Embodiment 2

[0076] The preparation of this embodiment has no carrier [ 78 The method of Br]MBrBG is as follows:

[0077] (1) Synthesis of 3-(trimethyltin base)-benzylguanidine shown in the formula A-II

[0078] Take 338mg (1mmol) of the bicarbonate of m-iodobenzylguanidine represented by the formula A-I and dissolve it in 15mL of DMF solution, then add 655mg (2mmol) of bis(trimethyltin) and mix well, and dissolve the whole Add 114mg (0.1mmol) of tetrakis(triphenylphosphine)palladium to 30mL of tetrahydrofuran, control the temperature at 70°C and carry out stille organotin reaction until the solution turns black and the color of the solution no longer deepens, spin dry to prepare The above-mentioned solution obtained, take chloroform to dissolve the residue after spin-drying, then wash the solution with water, spin-dry again, take methanol to dissolve the residue after spin-drying again, then wash the solution with n-hexane, and then dry, The 3-(trimethyltin base)-benzylguanidine represe...

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Abstract

The invention discloses a preparation method of carrier-free meta-halogen benzylguanidine [*X]MXBG; by taking bicarbonate of metaiodobenzylguanidine as a raw material, rational reaction conditions are designed, a tin precursor of the target compound carrier-free [*X]MXBG is obtained by one step, the reaction conditions are mild, steps are simple and convenient, the yield is relatively high, the labeling rate reaches more than 80%, and superfluous impurity groups are not introduced, and follow-up carrier-free [*X]MXBG synthesis is facilitated. The technical problems that carrier-free [*X] MXBG has low labeling rate, low yield, complex steps and a lot of impurities in the prior art are solved.

Description

technical field [0001] The invention belongs to the field of radiopharmaceutical preparation, in particular to a preparation method of carrier-free [*X]MXBG. Background technique [0002] Meta-iodobenzylguanidine (MIBG) belongs to the analogues of guanethidine, which can be concentrated in the adrenal medulla and is a homologue of the norepinephrine neurotransmitter (NE), with the help of which, it can be enriched for sympathetic Absorbed by nerve cells, it is a very valuable carrier in the diagnosis and treatment of myocardial abnormalities and neuroendocrine tumors. widely used in the prior art to 131 I-labeled MIBG for imaging and diagnosis and treatment of neuroendocrine tumors. [0003] Now clinically used abroad 131 I] MIBG is mostly passed 131 I and MIBG are prepared by the method of isotope exchange. The medicine prepared by this method contains a large amount of unlabeled MIBG carrier, not only the labeling rate is low, but also a large number of clinical trials...

Claims

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Application Information

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IPC IPC(8): C07B59/00C07C277/08C07C279/06
Inventor 王刚陈志明吴二明汪洋黄荷云
Owner JIANGSU INST OF NUCLEAR MEDICINE
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